pp2a

DT-061, an orally bioavailable protein phosphatase 2A (PP2A) activator, may be used in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Okadaic acid is a potent polyether marine toxin that accumulates in the digestive glands of marine mollusks.Okadaic acid is a highly potent and selective protein phosphatase (PP) inhibitor, inhibiting PP1, PP2A, PP3, PP4, and PP5.Okadaic acid activates Wnt β-catenin signaling in human HepaRG cells. catenin signaling in human HepaRG cells.

Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride may cause sensitization. Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride promotes apoptosis in HepG2 (IC50= 62 μM) and SK-Hep1 (IC50= 151 μM) cells and inhibits protein phosphatase 2A.

Microcystin-LR (Cyanoginosin-LR) is a potent inhibitor of type 1 and type 2A protein phosphatases (PP1 and PP2A), with IC50s of 1.7 nM and 0.04 nM, respectively.

PP2A Cancerous-IN-1 is a potent inhibitor of CIP2A (Cancerous inhibitor of PP2A) and p-Akt, demonstrating significant anti-proliferative effects.

TPP2a is a mitochondrial thioredoxin reductase (TrxR) inhibitor.

MKI-1 (MASTL Kinase Inhibitor-1) is an inhibitor of MASTL (microtubule-associated serine threonine kinase-like, IC50= 9.9 μM). MKI-1 exerts radiosensitizer and antitumor activities through PP2A activation in breast cancer.

Endothall is a protein phosphatase 2A (PP2A) inhibitor, capable of inhibiting PP2A (IC50: 90 nM) and PP1 (IC50: 5 uM). It acts as a herbicide and can also be useful in cancer chemotherapy.

Calyculin A ((-)-Calyculin A), a toxicant in the Japanese marine sponge CDiscodermia calyxC, is a selective and potent inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), inducing hyperactivation of cryopreserved bovine spermatozoa and inhibiting radiation-induced gammaH2AX DNA repair disease in human lymphocytes. gammaH2AX DNA repair foci in human lymphocytes.

D-erythro-Sphingosine (trans-4-Sphingenine) is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator

(Rac)-LB-100, a novel Protein Phosphatase 2A (PP2A) inhibitor, sensitizes malignant meningioma cells to the therapeutic effects of radiation

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) shows human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity, with IC50 values of 0.83 + - 0.04 microM and 4.20 + - 0.19 microM, respectively.

LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.

IQ 1 has multiple roles, such as maintaining the multifunctionality of mouse ESCs, decreasing Wnt-stimulated phosphorylation, blocking PP2A Nkd interactions, and so on.

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

FTY720-Mitoxy is an FTY720 analog that can be uesd as a novel stimulator of the activity of the protein phosphatase 2A (PP2A), targeting mitochondria.

AMZ30 is a selective inhibitor of PME-1 (IC50: 600 nM). It also reduces the demethylated form of PP2A in living cells.

TAT-PDHPS1 is a peptide inhibitor targeting Yes-associated protein (YAP) signaling, composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. It operates by binding to protein phosphatase 2 phosphatase activator (PTPA), thereby activating protein phosphatase 2A (PP2A). This activation precipitates the phosphorylation of YAP, culminating in the suppression of genes targeted by YAP. Demonstrated to inhibit the proliferation of ovarian cancer cells in vitro and reduce ovarian tumor growth in a subcutaneous xenograft mouse model, TAT-PDHPS1 presents a potent approach to managing ovarian malignancies.

Rubratoxin A is a classical mycotoxin used as a PP2A-specific inhibitor.

ATUX-1215, a protein phosphatase 2A (PP2A) activator, diminishes the phosphorylation of ERK, p38, JNK, and Akt, as well as decreases the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals, potentially decelerating lung fibrosis progression [1].

ATUX-8385 is a potent activator of PP2A. It binds to the PR65 subunit and holds promise for research into cancer and chronic diseases, including Alzheimer's disease and chronic obstructive pulmonary disease (COPD).

Tautomycin is a potent and specific protein phosphatases 1 and 2A inhibitor (Kiapp of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively), and is an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus.

N-Stearoylsphingosine (Cer(d18:1 18:0)) is an amide compound widely found in eukaryotic organisms that enhances protein phosphatase 2A (PP2A) activity by interfering with the binding of PP2A to PP2A inhibitor 2, leading to dephosphorylation of Akt.N-Stearoylsphingosine is used in prostate cancer research.